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    Anticancer agents based on regulation of protein prenylation
    1.
    发明授权
    Anticancer agents based on regulation of protein prenylation 失效
    基于蛋白异戊烯化调节的抗癌剂

    公开(公告)号：US07423170B2

    公开(公告)日：2008-09-09

    申请号：US11275662

    申请日：2006-01-23

    申请人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    发明人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    IPC分类号： C07C69/007 ,  C07C69/017 ,  A01N57/14 ,  A01N41/04 ,  A01N41/10

    CPC分类号： A61K31/66 ,  A61K31/20 ,  C07C69/63 ,  C07C217/46 ,  C07C219/20 ,  C07D303/32 ,  C07D303/48 ,  C07F9/091

    摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

    摘要翻译： 已知当诸如Ras和RhoB的癌蛋白定位在癌细胞膜的内表面时，诸如Ras和RhoB的癌蛋白以无限制的方式诱导细胞分裂。 定位通过异戊烯化反应进行，由此在酶（例如法呢基蛋白转移酶）的存在下将疏水基团（例如法呢基）连接到蛋白质上。 因此，通过共价修饰来停用异戊烯基化酶可最终导致癌细胞生长的缓解和/或停止。 具有与异戊烯基化酶共价或基本上不可逆地键合的必需结构基团的各种异戊二烯基化抑制剂包括与疏水性底物模拟基团键合的羰基或硫代羰基化合物（或这些化合物的掩蔽型）和α氧代环氧化物。 羰基或硫代羰基化合物还含有核原子或基团以增强形成共价键的倾向。

    Anticancer agents based on regulation of protein prenylation
    3.
    发明授权
    Anticancer agents based on regulation of protein prenylation 失效
    基于蛋白异戊烯化调节的抗癌剂

    公开(公告)号：US07943665B2

    公开(公告)日：2011-05-17

    申请号：US12204585

    申请日：2008-09-04

    申请人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    发明人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    IPC分类号： A01N37/10

    CPC分类号： A61K31/66 ,  A61K31/20 ,  C07C69/63 ,  C07C217/46 ,  C07C219/20 ,  C07D303/32 ,  C07D303/48 ,  C07F9/091

    摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

    摘要翻译： 已知当诸如Ras和RhoB的癌蛋白定位在癌细胞膜的内表面时，诸如Ras和RhoB的癌蛋白以无限制的方式诱导细胞分裂。 定位通过异戊烯化反应进行，由此在酶（例如法呢基蛋白转移酶）的存在下将疏水基团（例如法呢基）连接到蛋白质上。 因此，通过共价修饰来停用异戊烯基化酶可最终导致癌细胞生长的缓解和/或停止。 具有与异戊烯基化酶共价或基本上不可逆地键合的必需结构基团的各种异戊二烯基化抑制剂包括与疏水性底物模拟基团键合的羰基或硫代羰基化合物（或这些化合物的掩蔽型）和α氧代环氧化物。 羰基或硫代羰基化合物还含有核原子或基团以增强形成共价键的倾向。

    ANTICANCER AGENTS BASED ON REGULATION OF PROTEIN PRENYLATION
    4.
    发明申请
    ANTICANCER AGENTS BASED ON REGULATION OF PROTEIN PRENYLATION 失效
    基于蛋白质预处理调控的反应剂

    公开(公告)号：US20090143467A1

    公开(公告)日：2009-06-04

    申请号：US12204585

    申请日：2008-09-04

    申请人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    发明人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    IPC分类号： A61K31/232 ,  C12Q1/48

    CPC分类号： A61K31/66 ,  A61K31/20 ,  C07C69/63 ,  C07C217/46 ,  C07C219/20 ,  C07D303/32 ,  C07D303/48 ,  C07F9/091

    摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

    摘要翻译： 已知当诸如Ras和RhoB的癌蛋白定位在癌细胞膜的内表面时，诸如Ras和RhoB的癌蛋白以无限制的方式诱导细胞分裂。 定位通过异戊烯化反应进行，由此在酶（例如法呢基蛋白转移酶）的存在下将疏水基团（例如法呢基）连接到蛋白质上。 因此，通过共价修饰来停用异戊烯基化酶可最终导致癌细胞生长的缓解和/或停止。 具有与异戊烯基化酶共价或基本上不可逆地键合的必需结构基团的各种异戊二烯基化抑制剂包括与疏水性底物模拟基团键合的羰基或硫代羰基化合物（或这些化合物的掩蔽型）和α氧代环氧化物。 羰基或硫代羰基化合物还含有核原子或基团以增强形成共价键的倾向。

    Modified chalcone compounds as antimitotic agents
    10.
    发明授权
    Modified chalcone compounds as antimitotic agents 有权
    改性查耳酮化合物作为抗生物剂

    公开(公告)号：US07714025B2

    公开(公告)日：2010-05-11

    申请号：US11744027

    申请日：2007-05-03

    申请人： Seth D. Rose ,  Rosemarie F. Hartman

    发明人： Seth D. Rose ,  Rosemarie F. Hartman

    IPC分类号： A61K31/16 ,  C07D231/10 ,  C07C49/00

    CPC分类号： C07C69/653 ,  C07C327/32 ,  C07D209/12 ,  C07D213/50 ,  C07D231/12 ,  C07D307/46 ,  C07D311/28

    摘要： Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.

    摘要翻译： 公开了包含改性查耳酮或改性查耳酮衍生物的抗微生物剂。 改性查耳酮或改性查耳酮衍生物化合物具有通式CHAL-LIN-COV，其中CHAL是查耳酮或查耳酮衍生物部分，LIN是任选的接头部分，COV是共价结合部分（例如，α，bgr ; - 不饱和巯基酯基）。 改性查耳酮或改性查耳酮衍生物化合物提供了一种改进的干扰微管蛋白聚合的方法，例如通过微管蛋白与共价结合部分之间的共价（且基本上不可逆）的结合，潜在地导致肿瘤大小和/或消失的降低 癌症，有利于癌症患者。